| 产品介绍 |
Tideglusib(NP-031112)是不可逆的非ATP竞争性GSK-3β抑制剂，IC50为60 nM。 |
| 备注 |
Tideglusib is an irreversible, non ATP-competitive GSK-3β inhibitor with IC50 of 60 nM; fails to inhibit kinases with a Cys homologous to Cys-199 located in the active site. Phase 1/2. |
| 生化机理 |
Tideglusib, also known as NP031112 or NP-12, is a potent non ATP-competitive inhibitor of glycogen synthase kinase-3 (GSK3), an important kinase studied in stem cell research and neurodegenerative diseases. It is currently in clinical trials for Alzheimer′s disease and Progressive Supranuclear Palsy (PSP). Tideglusib reduces phosphorylation of the tau protein and the accumulation of amyloid plaques, reduces hippocampal and entorhinal cortex neuron loss and improves spatial memory deficits. It has also shown neuroprotective and anti-inflammatory activity in a variety of animal models. |
| 别名 |
NP-12;NP031112;4-苄基-2-(萘-1-基)-[1,2,4]噻二唑烷-3,5-二酮;NP 031112;NP-031112;4-Benzyl-2-(naphthalen-1-yl)-[1,2,4]thiadiazolidine-3,5-dione |
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